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/ Gliquidone

格列喹酮 /Gliquidone {[allProObj[0].p_purity_real_show]}

货号：A559869 同义名： AR-DF 26

Gliquidone is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.

Gliquidone 化学结构 CAS号：33342-05-1
Gliquidone 化学结构
CAS号：33342-05-1
Gliquidone 3D分子结构
CAS号：33342-05-1
Gliquidone 化学结构 CAS号：33342-05-1
Gliquidone 3D分子结构 CAS号：33342-05-1
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Gliquidone 纯度/质量文件 产品仅供科研

货号：A559869 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Potassium Channel ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

 		97%
Dronedarone Hydrochloride ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		98%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

 		98%
Glibenclamide ✔ 98%
Amiodarone HCl ✔ 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

 		98%
Repaglinide ✔ 98%
Dofetilide ✔ 98%
Nateglinide ✔ 99%
Quinine hydrochloride dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

 		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Gliquidone 生物活性

靶点

  • Potassium Channel

    Potassium channel, IC50:27.2 nM
描述 Gliquidone, a sulfonylurea class drug used for treating diabetes mellitus type 2. Gliquidone reduced the body weight and the kidney weight/body weight ratio of mice. Gliquidone improved the kidney function, indicated by reductions in urinary protein, blood urea nitrogen, and serum creatinine and triglyceride. Gliquidone can ameliorate the diabetic symptoms of diabetic nephropathy through inhibiting Notch/Snail1 signaling pathway, improving anti-oxidative response and delaying renal interstitial fibrosis[3]. Gliquidone treatment effectively reduced urinary protein in GK rats with diabetic nephropathy by improving glomerular lesions and promoting tubular reabsorption[4]. Moreover, using gliquidone nanoparticles revealed ~2.5-fold increase in Cmax when taken orally in the form of hard gelatin capsules in comparison to free gliquidone. The developed strategy of gliquidone nanoparticles possess a keen potential for exhibiting anti-diabetic effect[5].

Gliquidone 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02476760 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT02475499 - Completed - Canada, Quebec ... 展开 >> Lady Davis Institute for Medical Research, Jewish General Hospital Montreal, Quebec, Canada, H3T1E2 收起 <<
NCT00568074 Diabetes Diab... 展开 >>etes Mellitus, Type 2 收起 << Phase 4 Completed - China, Shanghai ... 展开 >> Novo Nordisk Investigational Site Shanghai, Shanghai, China, 200025 Novo Nordisk Investigational Site Shanghai, Shanghai, China, 200433 China, Sichuan Novo Nordisk Investigational Site Chengdu, Sichuan, China, 610041 China Novo Nordisk Investigational Site Beijing, China, 100029 收起 <<

Gliquidone 参考文献

[1]Galeotti N, Ghelardini C, et al. Involvement of potassium channels in amitriptyline and clomipramine analgesia. Neuropharmacology. 2001;40(1):75-84.

[2]Ocana M, Del Pozo E, et al. Subgroups among mu-opioid receptor agonists distinguished by ATP-sensitive K+ channel-acting drugs. Br J Pharmacol. 1995 Mar;114(6):1296-302.

[3]Tian H, Yang J, Xie Z, Liu J. Gliquidone Alleviates Diabetic Nephropathy by Inhibiting Notch/Snail Signaling Pathway. Cell Physiol Biochem. 2018;51(5):2085-2097

[4]Ke JT, Li M, Xu SQ, et al. Gliquidone decreases urinary protein by promoting tubular reabsorption in diabetic Goto-Kakizaki rats. J Endocrinol. 2014;220(2):129-141. Published 2014 Jan 8

[5]Mohamed MS, Abdelhafez WA, Zayed G, Samy AM. Optimization, in-vitro Release and in-vivo Evaluation of Gliquidone Nanoparticles. AAPS PharmSciTech. 2019;21(2):35. Published 2019 Dec 26

Gliquidone 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL

Gliquidone 技术信息

CAS号33342-05-1
分子式C27H33N3O6S
分子量 527.632
别名 AR-DF 26
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 50 mg/mL(94.76 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

2% DMSO+corn oil 5 mg/mL

Tags: Gliquidone | 33342-05-1 | AR-DF 26 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Gliquidone 纯度/质量文件 | Gliquidone 亚型比较 | Gliquidone 生物活性 | Gliquidone 临床数据 | Gliquidone 参考文献 | Gliquidone 实验方案 | Gliquidone 技术信息

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